Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Elacridar (formerly GW-120918; GF-120918; GG-918; GW-0918; GF120918; GF120918; GW0918; GG918) is a 3rd generationl and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor that has the potential to overcome P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs such as doxorubicin. Elacridar has been used both in vitro and in vivo as a tool inhibitor of P-gp to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma.
ln Vitro |
Elacridar (0.001-1 μM; 2 h) reduces the viability of 786-O cells [2]. Elacridar (5 μM; 24 h) modulates P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines [2]. Elacridar (5 μM; 24 h) impacts 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells [2].
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ln Vivo |
Elacridar (100 mg/kg; intraperitoneally) distributes differently in the brain and plasma[1]. 1.19 Elacridar Plasma Pharmacokinetic Parameters in Mice[1]. AUC0-inf (μg·min/ml) 1460 90.3 161.4 F 0.22 0.013 1 Mice PO 100 mg/kg Mice IP 100 mg/kg Mice IV 2.5 mg/ kg CL/F (ml/min) 2.05 33.2 0.46 Vd/F (liter) 3.5 12.3 0.17 t1/2 (h) 20 4.3 4.4
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Cell Assay |
Cell Viability Assay[2]
Cell Types: 786-O cells Tested Concentrations: 2.5 and 5 μM Incubation Duration: 2 hrs (hours) Experimental Results: Dose-dependently inhibited cell viability of 786-O cells and demonstrated better inhibitory effect with sunitnib adding Western Blot Analysis[2] Cell Types: MCF-7, Caki-1, and 786-O cell lines Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells. Cell Viability Assay[2] Cell Types: MCF-7 and 786-O cell lines Tested Concentrations: 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependently increased 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells. |
Animal Protocol |
Animal/Disease Models: FVB wild-type mice[1].
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip)injection; 100 mg/kg once Experimental Results: Showd a higher concertation in brain than plasma except at 4 h after the dose. |
References |
[1]. Sane R, et al. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.
[2]. Sato H, et al. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells. Eur J Pharmacol. 2015 Jan 5;746:258-66. |
Molecular Formula |
C34H33N3O5
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Molecular Weight |
563.64
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CAS # |
143664-11-3
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SMILES |
O(C([H])([H])[H])C1=C(C([H])=C2C(=C1[H])C([H])([H])N(C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C1=C([H])C([H])=C([H])C3C(C4C([H])=C([H])C([H])=C(C=4N([H])C=31)OC([H])([H])[H])=O)=O)C([H])([H])C2([H])[H])OC([H])([H])[H]
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7742 mL | 8.8709 mL | 17.7418 mL | |
5 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL | |
10 mM | 0.1774 mL | 0.8871 mL | 1.7742 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.